Modification of novel oxazolidinone derivatives at C-5 side chain and their antibacterial activities.
- Author:
Xin ZHAI
1
;
Guo-Gang ZHANG
;
Dong-Hui GOU
;
Jun-Peng LIU
;
Ping GONG
Author Information
- Publication Type:Journal Article
- MeSH: Anti-Bacterial Agents; chemical synthesis; chemistry; pharmacology; Microbial Sensitivity Tests; Molecular Structure; Oxazolidinones; chemical synthesis; chemistry; pharmacology; Staphylococcus aureus; drug effects; Structure-Activity Relationship
- From: Acta Pharmaceutica Sinica 2006;41(10):985-989
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo modify the C-5 side chains of the oxazolidinone derivatives and evaluate their in vitro antibacterial activities preliminarily.
METHODSThe title compounds were synthesized in 9 - 12 steps with the starting material 3-fluoroaniline and their in vitro antibacterial activities were examined by using Mueller-Hinton broth dilution method.
RESULTSThirty new compounds were designed and synthesized, in which eighteen novel title compounds were prepared and their structures were confirmed by 1H NMR and ESI-MS. Eleven compounds showed antibacterial activities to a certain extent, among them compounds 7a, 9a and 11a displayed promising activity.
CONCLUSIONCompounds 7a, 9a and 11a were worth further studying.
